Synthesis, Biological Activity, and ADME Properties of Novel S??DABOs/N??DABOs as HIV Reverse Transcriptase Inhibitors

…, G Casaluce, C Zamperini, E Dreassi, G Maga…

文献索引：Radi, Marco; Pagano, Mafalda; Franchi, Luigi; Castagnolo, Daniele; Schenone, Silvia; Casaluce, Gianni; Zamperini, Claudio; Dreassi, Elena; Maga, Giovanni; Samuele, Alberta; Gonzalo, Encarna; Clotet, Bonaventura; Este, Jose A.; Botta, Maurizio ChemMedChem, 2012 , vol. 7, # 5 p. 883 - 896

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被引用次数: 12

摘要

Abstract Previous studies aimed at exploring the SAR of C2-functionalized S-DABOs demonstrated that the substituent at this position plays a key role in the inhibition of both wild- type RT and drug-resistant enzymes, particularly the K103N mutant form. The introduction of a cyclopropyl group led us to the discovery of a potent inhibitor with picomolar activity against wild-type RT and nanomolar activity against many key mutant forms such as ...